CA2860008C - Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators - Google Patents

Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators Download PDF

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Publication number
CA2860008C
CA2860008C CA2860008A CA2860008A CA2860008C CA 2860008 C CA2860008 C CA 2860008C CA 2860008 A CA2860008 A CA 2860008A CA 2860008 A CA2860008 A CA 2860008A CA 2860008 C CA2860008 C CA 2860008C
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Prior art keywords
mmol
title compound
tetraaza
hplc
uplc
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CA2860008A
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English (en)
French (fr)
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CA2860008A1 (en
Inventor
Dominique Swinnen
Cyril Montagne
Vincent Pomel
Anna Quattropani
Jerome Molette
Patrick Gerber
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Merck Patent GmbH
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Merck Patent GmbH
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Publication date
Priority claimed from EP11195214.9A external-priority patent/EP2607364A1/en
Priority claimed from EP12171415.8A external-priority patent/EP2674434A1/en
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CA2860008A1 publication Critical patent/CA2860008A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2860008A 2011-12-22 2012-11-30 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators Active CA2860008C (en)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161578931P 2011-12-22 2011-12-22
EP11195214.9 2011-12-22
EP11195214.9A EP2607364A1 (en) 2011-12-22 2011-12-22 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators
US61/578,931 2011-12-22
US201261657978P 2012-06-11 2012-06-11
EP12171415.8A EP2674434A1 (en) 2012-06-11 2012-06-11 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators
US61/657,978 2012-06-11
EP12171415.8 2012-06-11
PCT/EP2012/004968 WO2013091773A1 (en) 2011-12-22 2012-11-30 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators

Publications (2)

Publication Number Publication Date
CA2860008A1 CA2860008A1 (en) 2013-06-27
CA2860008C true CA2860008C (en) 2020-11-10

Family

ID=48667735

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2860008A Active CA2860008C (en) 2011-12-22 2012-11-30 Tetraaza-cyclopenta[a]indenyl and their use as positive allosteric modulators

Country Status (8)

Country Link
US (1) US9403835B2 (enExample)
EP (1) EP2794608B1 (enExample)
JP (1) JP6112316B2 (enExample)
CN (1) CN104039789B (enExample)
AU (1) AU2012357169B2 (enExample)
CA (1) CA2860008C (enExample)
ES (1) ES2606839T3 (enExample)
WO (1) WO2013091773A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2813505A1 (en) * 2013-06-14 2014-12-17 Asceneuron SA Tetraaza-cyclopenta[a]indenyl derivatives
GB201317363D0 (en) 2013-10-01 2013-11-13 Eisai Ltd Novel compounds
US9844549B2 (en) 2014-08-26 2017-12-19 Astellas Pharma Inc. 2-aminothiazole derivative or salt thereof
UA123262C2 (uk) * 2015-02-11 2021-03-10 Суновіон Фармасьютикалз Інк. ЗШИТІ ДИГІДРО-4H-ПІРАЗОЛО[5,1-c][1,4]ОКСАЗИНІЛОВІ СПОЛУКИ І АНАЛОГИ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАНЬ ЦНС
WO2017038650A1 (ja) * 2015-08-28 2017-03-09 積水メディカル株式会社 ベンジル化合物
EA201990399A1 (ru) 2016-07-29 2019-07-31 Суновион Фармасьютикалз, Инк. Соединения, композиции и их применение
CN111183138A (zh) 2017-08-02 2020-05-19 赛诺维信制药公司 异色满化合物以及用途
BR112020012197A2 (pt) 2017-12-21 2020-11-24 Ribon Therapeutics Inc. quinazolinonas como inibidores de parp14

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2441926A1 (en) * 2001-03-27 2002-10-03 Neurogen Corporation (oxo-pyrazolo[1,5a]pyrimidin-2-yl)alkyl-carboxamides
MX2007006896A (es) * 2004-12-15 2007-06-26 Hoffmann La Roche Fenil-metanonas bi- y triciclicas sustituidas como inhibidores del transportador 1 de glicina (glyt-1) para el tratamiento de la enfermedad de alzheimer.
JP5232160B2 (ja) * 2006-11-14 2013-07-10 メルク・シャープ・アンド・ドーム・コーポレーション 糖尿病の治療又は予防のためのジペプチジルペプチダーゼivインヒビターとしての三環式芳香族複素環化合物
WO2011137049A1 (en) * 2010-04-30 2011-11-03 Merck Sharp & Dohme Corp. Heterocyclic quinolizine derived m1 receptor positive allosteric modulators
EP2813505A1 (en) * 2013-06-14 2014-12-17 Asceneuron SA Tetraaza-cyclopenta[a]indenyl derivatives

Also Published As

Publication number Publication date
ES2606839T3 (es) 2017-03-28
JP6112316B2 (ja) 2017-04-12
US9403835B2 (en) 2016-08-02
CN104039789A (zh) 2014-09-10
EP2794608B1 (en) 2016-09-14
US20150018343A1 (en) 2015-01-15
AU2012357169A1 (en) 2014-08-07
JP2015502371A (ja) 2015-01-22
AU2012357169B2 (en) 2017-03-30
CN104039789B (zh) 2016-09-07
WO2013091773A1 (en) 2013-06-27
EP2794608A1 (en) 2014-10-29
CA2860008A1 (en) 2013-06-27

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